CO2018007271A2 - New derivatives of phosphinanes and azaphosphinans, their preparation process and the pharmaceutical compositions containing them - Google Patents

New derivatives of phosphinanes and azaphosphinans, their preparation process and the pharmaceutical compositions containing them

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Publication number
CO2018007271A2
CO2018007271A2 CONC2018/0007271A CO2018007271A CO2018007271A2 CO 2018007271 A2 CO2018007271 A2 CO 2018007271A2 CO 2018007271 A CO2018007271 A CO 2018007271A CO 2018007271 A2 CO2018007271 A2 CO 2018007271A2
Authority
CO
Colombia
Prior art keywords
azaphosphinans
phosphinanes
pharmaceutical compositions
preparation process
compositions containing
Prior art date
Application number
CONC2018/0007271A
Other languages
Spanish (es)
Inventor
Philippe Gloanec
Arnaud-Pierre Schaffner
Patricia Sansilvestri-Morel
Alain Rupin
Philippe Mennecier
Marie-Odile Vallez
Original Assignee
Servier Lab
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=55752640&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CO2018007271(A2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Servier Lab filed Critical Servier Lab
Publication of CO2018007271A2 publication Critical patent/CO2018007271A2/en

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/66Phosphorus compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/66Phosphorus compounds
    • A61K31/675Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6564Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
    • C07F9/6568Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus atoms as the only ring hetero atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6564Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
    • C07F9/6581Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and nitrogen atoms with or without oxygen or sulfur atoms, as ring hetero atoms
    • C07F9/6584Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and nitrogen atoms with or without oxygen or sulfur atoms, as ring hetero atoms having one phosphorus atom as ring hetero atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6564Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
    • C07F9/6581Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and nitrogen atoms with or without oxygen or sulfur atoms, as ring hetero atoms
    • C07F9/6584Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and nitrogen atoms with or without oxygen or sulfur atoms, as ring hetero atoms having one phosphorus atom as ring hetero atom
    • C07F9/65842Cyclic amide derivatives of acids of phosphorus, in which one nitrogen atom belongs to the ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6564Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
    • C07F9/6581Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and nitrogen atoms with or without oxygen or sulfur atoms, as ring hetero atoms
    • C07F9/6584Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and nitrogen atoms with or without oxygen or sulfur atoms, as ring hetero atoms having one phosphorus atom as ring hetero atom
    • C07F9/65842Cyclic amide derivatives of acids of phosphorus, in which one nitrogen atom belongs to the ring
    • C07F9/65846Cyclic amide derivatives of acids of phosphorus, in which one nitrogen atom belongs to the ring the phosphorus atom being part of a six-membered ring which may be condensed with another ring system

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Dermatology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Compuestos de fórmula (I) (ver imágen adjunto) en la que: Ak1 representa una cadena alquilo, X representa -(CH2)m-, -CH(R)-, -N(R)-, -CH2-N(R)-, –N(R)-CH2- o -CH2-N(R)-CH2-, m y R son tales como se han definido en la descripción, R1 y R2 representan cada uno H cuando X representa -(CH2)m-, -CH(R)-, -N(R)-, -CH2-N(R)- o –N(R)-CH2-, o bien forman juntos una unión cuando X representa -CH2-N(R)-CH2-, R3 representa NH2, Cy-NH2, Cy-Ak3-NH2 o piperidin-4-ilo, Cy y Ak3 son tales como se han definido en la descripción, R4 y R5, idénticos o diferentes, representan cada uno H o F, sus isómeros ópticos, así como sus sales de adición a un ácido farmacéuticamente aceptable. Medicamentos.Compounds of formula (I) (see attached image) in which: Ak1 represents an alkyl chain, X represents - (CH2) m-, -CH (R) -, -N (R) -, -CH2-N (R ) -, -N (R) -CH2- or -CH2-N (R) -CH2-, m and R are as defined in the description, R1 and R2 each represent H when X represents - (CH2) m -, -CH (R) -, -N (R) -, -CH2-N (R) - or –N (R) -CH2-, or together form a joint when X represents -CH2-N (R) -CH2-, R3 represents NH2, Cy-NH2, Cy-Ak3-NH2 or piperidin-4-yl, Cy and Ak3 are as defined in the description, R4 and R5, identical or different, each represent H or F, its optical isomers, as well as its addition salts to a pharmaceutically acceptable acid. Medicines.

CONC2018/0007271A 2016-01-14 2018-07-12 New derivatives of phosphinanes and azaphosphinans, their preparation process and the pharmaceutical compositions containing them CO2018007271A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
FR1670004A FR3046793B1 (en) 2016-01-14 2016-01-14 NOVEL PHOSPHINAN DERIVATIVES AND AZAPHOSPHINANES, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
PCT/FR2017/050075 WO2017121969A1 (en) 2016-01-14 2017-01-13 Novel phosphinane and azaphosphinane derivatives, method for preparing same and pharmaceutical compositions containing same

Publications (1)

Publication Number Publication Date
CO2018007271A2 true CO2018007271A2 (en) 2018-07-19

Family

ID=55752640

Family Applications (1)

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CONC2018/0007271A CO2018007271A2 (en) 2016-01-14 2018-07-12 New derivatives of phosphinanes and azaphosphinans, their preparation process and the pharmaceutical compositions containing them

Country Status (47)

Country Link
US (2) US10138260B2 (en)
EP (1) EP3271368B1 (en)
JP (1) JP2019504070A (en)
KR (1) KR20180101522A (en)
CN (1) CN108495857A (en)
AR (1) AR107433A1 (en)
AU (1) AU2017207003B2 (en)
BR (1) BR112018014020A2 (en)
CA (1) CA3011184C (en)
CL (1) CL2018001862A1 (en)
CO (1) CO2018007271A2 (en)
CU (1) CU20180072A7 (en)
CY (1) CY1121154T1 (en)
DK (1) DK3271368T3 (en)
DO (1) DOP2018000165A (en)
EA (1) EA035072B1 (en)
EC (1) ECSP18051972A (en)
ES (1) ES2709376T3 (en)
FR (1) FR3046793B1 (en)
GE (1) GEP20207092B (en)
HK (1) HK1244283B (en)
HR (1) HRP20190193T1 (en)
HU (1) HUE042924T2 (en)
IL (1) IL260425B (en)
JO (1) JO3660B1 (en)
LT (1) LT3271368T (en)
MA (1) MA41798B1 (en)
MD (1) MD3271368T2 (en)
ME (1) ME03305B (en)
MX (1) MX367319B (en)
NI (1) NI201800073A (en)
PE (1) PE20181503A1 (en)
PH (1) PH12018501373A1 (en)
PL (1) PL3271368T3 (en)
PT (1) PT3271368T (en)
RS (1) RS58338B1 (en)
RU (1) RU2729641C2 (en)
SG (1) SG11201805757WA (en)
SI (1) SI3271368T1 (en)
SV (1) SV2018005721A (en)
TN (1) TN2018000226A1 (en)
TR (1) TR201820430T4 (en)
TW (1) TWI625334B (en)
UA (1) UA121275C2 (en)
UY (1) UY37072A (en)
WO (1) WO2017121969A1 (en)
ZA (1) ZA201804391B (en)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR3046793B1 (en) * 2016-01-14 2018-01-05 Les Laboratoires Servier NOVEL PHOSPHINAN DERIVATIVES AND AZAPHOSPHINANES, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

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MXPA03001425A (en) * 2000-08-17 2003-06-06 Pfizer PHARMACEUTICAL COMPOUNDS.
SE0103272D0 (en) * 2001-09-28 2001-09-28 Astrazeneca Ab Chemical compounds
WO2003076416A1 (en) * 2002-03-08 2003-09-18 Warner-Lambert Company Llc Oxo azabicyclic compounds
US7420000B2 (en) * 2003-09-10 2008-09-02 University Of Southern California Amino phosphonate and amino bis-phosphonate derivatives
US20050143349A1 (en) * 2003-12-17 2005-06-30 Quatrx Pharmaceuticals Co. Phosphorus containing compounds useful for the regulation of LDL and Lp(a) levels
CA2604912A1 (en) * 2005-04-18 2006-10-26 Bayer Schering Pharma Aktiengesellschaft Use of tafi inhibitors for enhanced myocardial reperfusion and facilitated pci
JP5478488B2 (en) * 2007-06-20 2014-04-23 メルク・シャープ・アンド・ドーム・コーポレーション JANUS kinase inhibitors
FR2920773B1 (en) * 2007-09-11 2009-10-23 Servier Lab 1,2,4,5-TETRAHYDRO-3H-BENZAZEPINES DERIVATIVES, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
FR2947266B1 (en) * 2009-06-26 2011-06-17 Servier Lab NOVEL 2-MERCAPTOCYCLOPENTANECARBOXYLIC ACID DERIVATIVES, PROCESS FOR PREPARING THEM AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME
PT2507249E (en) * 2009-09-09 2016-02-15 Gilead Sciences Inc Inhibitors of flaviviridae viruses
JP6186434B2 (en) * 2012-07-18 2017-08-23 サンシャイン・レイク・ファーマ・カンパニー・リミテッドSunshine Lake Pharma Co.,Ltd. Nitrogen heterocyclic derivatives and their applications in medicine
FR3046793B1 (en) * 2016-01-14 2018-01-05 Les Laboratoires Servier NOVEL PHOSPHINAN DERIVATIVES AND AZAPHOSPHINANES, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

Also Published As

Publication number Publication date
ME03305B (en) 2019-10-20
AU2017207003B2 (en) 2020-10-08
CU20180072A7 (en) 2018-10-04
EP3271368B1 (en) 2018-10-31
ZA201804391B (en) 2020-01-29
AU2017207003A2 (en) 2018-10-04
SV2018005721A (en) 2018-09-06
AU2017207003A1 (en) 2018-07-26
US10138260B2 (en) 2018-11-27
CN108495857A (en) 2018-09-04
ECSP18051972A (en) 2018-07-31
DK3271368T3 (en) 2019-02-25
FR3046793A1 (en) 2017-07-21
TW201726697A (en) 2017-08-01
EP3271368A1 (en) 2018-01-24
PH12018501373B1 (en) 2019-02-27
HUE042924T2 (en) 2019-07-29
TWI625334B (en) 2018-06-01
PH12018501373A1 (en) 2019-02-27
MA41798B1 (en) 2018-11-30
FR3046793B1 (en) 2018-01-05
MX2018008639A (en) 2018-11-19
CA3011184C (en) 2020-09-29
EA201891599A1 (en) 2019-01-31
RU2018129027A (en) 2020-02-14
WO2017121969A1 (en) 2017-07-20
MD3271368T2 (en) 2019-03-31
ES2709376T3 (en) 2019-04-16
BR112018014020A2 (en) 2018-12-11
DOP2018000165A (en) 2018-09-15
AR107433A1 (en) 2018-05-02
JO3660B1 (en) 2020-08-27
IL260425B (en) 2020-05-31
US20180016288A1 (en) 2018-01-18
EA035072B1 (en) 2020-04-23
HRP20190193T1 (en) 2019-04-05
KR20180101522A (en) 2018-09-12
HK1244283B (en) 2019-11-22
RS58338B1 (en) 2019-03-29
US10654878B2 (en) 2020-05-19
GEP20207092B (en) 2020-04-10
RU2729641C2 (en) 2020-08-11
RU2018129027A3 (en) 2020-03-19
CL2018001862A1 (en) 2018-10-05
SG11201805757WA (en) 2018-08-30
PT3271368T (en) 2018-12-04
PE20181503A1 (en) 2018-09-18
TR201820430T4 (en) 2019-01-21
CY1121154T1 (en) 2020-05-29
US20190031693A1 (en) 2019-01-31
JP2019504070A (en) 2019-02-14
MX367319B (en) 2019-08-15
UA121275C2 (en) 2020-04-27
PL3271368T3 (en) 2019-04-30
UY37072A (en) 2017-07-31
NI201800073A (en) 2018-09-06
SI3271368T1 (en) 2019-02-28
TN2018000226A1 (en) 2019-10-04
CA3011184A1 (en) 2017-07-20
MA41798A (en) 2018-01-24
LT3271368T (en) 2018-12-10

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